Detoxicant



' therapeutic and the other toxic.

as its therapeutic eiiect.

to provide a therapeutic agent comprising in Patented Nov. 28, 1944 pn'roxicnnr Gustav J. Martin. Elmhurst, and Marvin R.

Thompson. Great Neck, N. Y., assignors to William R. Warner & Company, Inc., New York, N. Y., a corporation of Delaware No Drawing. Application May 2, 1940,

Serial No. 332,986

4 Claims.

This invention relates to therapeutic materials of lowered toxicity. More particularly, it relates to therapeutic agents comprising Atophan" and similar compounds in admixture with a material lowering the toxicity thereof.

Atophan" '(phenylquinoline carboxylic acid) is a drug used in the treatment of rheumatism, gout andsimilar diseases of the human body. The amount of the drug that may be administered, however, is usually less than the amount that would obtain the maximum, or in many cases a desirable, therapeutic effect. This limit is occasioned by the toxic action of the Atophan."

It is an object of our invention; to provide a therapeutic agent comprising Atophan, its re lated and similarly acting derivatives and compounds, such as novatophan, and atoquinol, which are non-toxic or of reduced toxicity and which canbe administered in greater amounts in most cases, or at least in the usual amounts without an abjectionable toxic eflect on the hu combination Atophan" and related and similarly acting compounds and derivatives with cysteine and their equivalents, i. e., their precursors and" ascorbic acidin either a dry mixture or in soluetc.

tion. This mixture may then be administered in the same way that Atophan is normally administered, namely, orally, parenterally, rectally, While the cysteine alone or the cysteine and ascorbic acid may be administered to the human body separately from the Atophan," we find it moreconvenient to administer them as a mixture since this assures that the proper amount of both ingredients will be administered at the same time, and also eliminates the necessity for administering two drugs which would be less convenient and might give rise to misunderstanding as to the amount and nature of the drugs described have two characteristics, one,

I It would be relatively simple to modify the drug or the action 01 the drug so as to alter its toxic as well However, it is not a simple matterto alter one of these characteristics without altering the other, i, e., to alter the toxicity without destroying the therapeutic effect.

The action and theory of detoxication has been appreciated heretofore, and in general, a detoxifying material is'thought to combine or coact with the drug in the bod in such a manner as to mask the toxic characteristic while leaving unaltered the structural characteristic of the compound that is responsible for the therapeutic eflect. But the exact action of various materials is little known, and the nature of detoxicants or their action with a particular drug so as not to affect its therapeutic effect cannot be predicted from any available knowledge.

We have discovered that if cysteine or an equivalent compound is administered at the same of the Atophan" is not appreciably interfered with. The inclusion of .ascorbic acid with the cysteine gives somewhat more effective results than cysteine alone or than ascorbic acid alone.

It is a further object of our invention therefore administration.

Upon being taken into the body, the Atophan" or related compound and cysteine or the cysteine and ascorbic acid coact or react to produce a material having the non-toxic, therapeutic effect. If desired, the Atophan and ascorbic acid and/or cysteine may be reacted in the-laboratory in a manner similar to the action that takes place in the body in order to provide a single new compound which may be administered to produce the non-toxic therapeutic effect, the ascorbic acid conjugate having the approximate composition C22H1'IO7N, while the cysteine conjugate is represented by CmH'1sO4N2S. Both are hitherto unknown compounds.

hanced results are not obtained. amounts of cysteine or cysteine and ascorbic acid The proportions of the materials are not criti cal, since both cysteine and ascorbic acid are found in and formed fromdietary components and may therefore be viewed as a food for the human body. They may'be taken/into the body in relatively large amounts without any harmful action. The upper limit of the proportion of cysteine in our composition is therefore very high, although as a practical matter, in most instances, there is a maximum amount beyond which en- Very small also obtain improved results, and there is no min; imum below which some improvement is not obtained. -The proportions may also vary somewhat depending upon the tolerances and peculiarities of the patient with respect to the Atophan. In general, however, we find a mix- .therapeutic material having superior and advantageous non-toxic properties, as described in the specification and following claims forming a part thereof.

We claim:

1. A therapeutic agent for usein connection with the treatment of rheumatism, gout and similar ailments including Atop'han for combating said ailments, in association with cysteine and an ascorbic acid to lower the toxicity of said Atophan without materially impairing th therapeutic effect thereof.

2. A therapeutic agent for use in connection with the treatment of rheumatism, gout and similar ailments including Atophan. for combating said ailments, in association with cysteine to lower thetoxicity of said Atophan" without materially impairing, the therapeutic. eflect thereof.

3.A therapeutic agent for use in connection with the treatment of rheumatism, gout and similar ailments, comprising a compound selected.

from the group consisting of phenylcinchoninic acid and its esters, for combating said ailments,

- in association with cysteine and an ascorbic acid to lower the toxicity oi saidcompound without materially impairing the therapeutic eflect 7 thereof.

.4. A therapeutic agent for use in connection with the treatment 0! rheumatism, gout and simi- GUSTAV J. MARTIN. MARVIN a.- THOMPSON. 

